The drug 5-azacytidine is currently being evaluated against a resistant form of leukemia. Due to the side effects of nausea and vomiting, which limit the dose, it is a preferred method of treatment to infuse the drug slowly. However, the instability of the drug and thereby its subsequent loss is a serious drawback to the infusion.
Even when the drug is infused in lactated Ringer injection technique, which provides optimum stability conditions for the drug at pH 6.4, about 10% of the drug is lost in 2 hours at room temperature.
What is required is a means to stabilize the drug. The creation of a pro-drug form has several requirements. The stability in the pro-drug form must last the requisite infusion time. Secondly, the pro-drug form must be free of toxicity. Thirdly, the active drug form must be released under physiological conditions.
The present invention presents a means to meet these requirements in a safe and acceptable manner.